1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Adrenergic Receptor

Adrenergic Receptor

Beta Receptor

Adrenergic receptors are a class of G protein-coupled receptors that are targets of the catecholamines, especially norepinephrine and epinephrine. Many cells possess these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system. The sympathetic nervous system is responsible for the fight-or-flight response, which includes widening the pupils of the eye, mobilizing energy, and diverting blood flow from non-essential organs to skeletal muscle. There are two main groups of adrenergic receptors, α and β, with several subtypes. α receptors have the subtypes α1 and α2. β receptors have the subtypes β1, β2 and β3. All three are linked to Gs proteins, which in turn are linked to adenylate cyclase. Agonist binding thus causes a rise in the intracellular concentration of the second messenger cAMP. Downstream effectors of cAMP include cAMP-dependent protein kinase (PKA), which mediates some of the intracellular events following hormone binding.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B1270R
    Isoxsuprine hydrochloride (Standard)
    Agonist
    Isoxsuprine hydrochloride (Standard) is the analytical standard of Isoxsuprine hydrochloride. This product is intended for research and analytical applications. Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
    Isoxsuprine hydrochloride (Standard)
  • HY-B0006S2
    Carvedilol-d5
    Inhibitor
    Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
    Carvedilol-d<sub>5</sub>
  • HY-13458S1
    Droxidopa-13C2,15N hydrochloride
    Droxidopa-13C2,15N (hydrochloride) is deuterium labeled Droxidopa. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a proagent to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood-brain barrier.
    Droxidopa-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N hydrochloride
  • HY-119006
    L-640,033
    Agonist
    L-640,033 is a potent agonist of β-adrenergic. L-640,033 play an important role in lipid metabolism, and growth.
    L-640,033
  • HY-135895
    Detomidine carboxylic acid
    Agonist
    Detomidine carboxylic acid is the major urinary metabolite of Detomidine. Detomidine is a synthetic α2-adrenergic agonist. Detomidine also has cardiac and respiratory effects and an antidiuretic action.
    Detomidine carboxylic acid
  • HY-A0007R
    Rotigotine Hydrochloride (Standard)
    Antagonist
    Rotigotine (Hydrochloride) (Standard) is the analytical standard of Rotigotine (Hydrochloride). This product is intended for research and analytical applications. Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
    Rotigotine Hydrochloride (Standard)
  • HY-136693
    L-654284
    L-654284 is an α2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for α2 and α1 adrenergic receptors, and exhibits a Ki of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing α2-adrenergic receptor blocking activity in the central nervous system.
    L-654284
  • HY-100255
    Tiodazosin
    Antagonist
    Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist.
    Tiodazosin
  • HY-101338A
    RS-79948-197 hemihydrate
    Antagonist 99.5%
    RS-79948-197 hemihydrate is a non-imidazoline α2-adrenoceptor antagonist. RS-79948-197 hemihydrate shows Kd values of 0.42 nM, 0.18 nM, 0.19 nM, 0.60 nM, 0.46 nM, and 0.77 nM for rat α2A, rat α2B, rat α2C, human α2A, human α2B, and human α2C, respectively.
    RS-79948-197 hemihydrate
  • HY-P1442
    AdTx1
    Antagonist
    AdTx1 is a selective α1A-adrenoceptor antagonist (Ki: 0.35 nM). AdTx1 can be used for research of benign prostatic hyperplasia.
    AdTx1
  • HY-106769
    Fluparoxan
    Antagonist 99.66%
    Fluparoxan is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan is an anti-depressant agent.
    Fluparoxan
  • HY-158194
    α2C adrenoceptor agonist 1
    Agonist
    α2C adrenoceptor agonist 1 (Compound A) is an orally active, highly selective, and non-central nervous system penetrating agonist for the α2C-adrenoceptor, with EC50 and Ki values of 108 nM and 12 nM, respectively. α2C adrenoceptor agonist 1 can be used in the study of nasal congestion.
    α2C adrenoceptor agonist 1
  • HY-175289
    hERG-IN-3
    Inhibitor
    hERG-IN-3 is an orally active hERG blocker with an IC50 of 44.5 nM. hERG-IN-3 exhibits a Ki for β2-adrenergic receptor of 14 nM. hERG-IN-3 exhibits the skeletal muscle Nav1.4 and sodium channel-blocking activities (IC50 = 4.4 μM, 3-fold increasement than hNav1.5). hERG-IN-3 displays a potent antimyotonic activity in an animal model. hERG-IN-3 can be used for the study of Myotonia Congenita.
    hERG-IN-3
  • HY-17380R
    (S)-Timolol maleate (Standard)
    Antagonist
    (S)-Timolol (maleate) (Standard) is the analytical standard of (S)-Timolol (maleate). This product is intended for research and analytical applications. (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction.
    (S)-Timolol maleate (Standard)
  • HY-B0010DR
    Arformoterol tartrate (Standard)
    Agonist
    Arformoterol (tartrate) (Standard) is the analytical standard of Arformoterol (tartrate). This product is intended for research and analytical applications. Arformoterol ((R,R)-Formoterol) tartrate, the (R,R)-enantiomer of Formoterol, is a long-acting β2-adrenergic receptor (β2-AR) agonist, with a Kd of 2.9 nM. Arformoterol tartrate can be used for the research of chronic obstructive pulmonary disease (COPD).
    Arformoterol tartrate (Standard)
  • HY-15780A
    Brexpiprazole hydrochloride
    Agonist
    Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
    Brexpiprazole hydrochloride
  • HY-103209
    Rec 15/2615 hydrochloride
    Antagonist
    Rec 15/2615 hydrochloride is a potent and selective α-1B adrenoceptor antagonist with Ki values of 1.9 nM, 0.3 nM, 2.6 nM for α1A, α1B, α1D, respectively. Rec 15/2615 hydrochloride modulates vaginal smooth muscle contractility and genital engorgement.
    Rec 15/2615 hydrochloride
  • HY-103202
    SNAP5089 hydrochloride
    Antagonist
    SNAP5089 (hydrochloride) is a selective α1A adrenergic receptor antagonist. SNAP5089 (hydrochloride) can be used in the research of hypertension and benign prostatic hyperplasia.
    SNAP5089 hydrochloride
  • HY-B0976AR
    Fenoterol hydrobromide (Standard)
    Agonist
    Fenoterol (hydrobromide) (Standard) is the analytical standard of Fenoterol (hydrobromide). This product is intended for research and analytical applications. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research.
    Fenoterol hydrobromide (Standard)
  • HY-B0702S
    Nicergoline-13C,d3
    Inhibitor
    Nicergoline-13C,d3 is the 13C- and deuterium labeled Nicergoline. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease.
    Nicergoline-<sup>13</sup>C,d<sub>3</sub>
Cat. No. Product Name / Synonyms Application Reactivity

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